Abstract

Different anti-obesity drugs have proved unsuccessful due to their adverse effects. As a consequence, there is a growing interest in herbal remedies, with the aim to find new well-tolerated effective drugs. Leopoldia comosa (L.) Parl. grows in Central and Southern Europe, Northern Africa and Central and South-Western Asia, and the bulbs have been commonly used for food throughout history. In this study the effectiveness of L. comosa (L.) Parl. leaves and inflorescences hydroalcoholic extracts and fractions was verified through the evaluation of pancreatic lipase inhibitory activity. The metabolite profiling and the antioxidant activity were also investigated. Chemical composition of L. comosa leaves and inflorescences was assessed by means of GC–MS and HPTLC analyses. The ethyl acetate fraction of leaves sample showed the best antioxidant activity, tested through DPPH and β-carotene bleaching test. The effects on pancreatic lipase activity were assessed through the in vitro evaluation of the capacity to prevent p-nitrophenyl caprylate hydrolysis. Interestingly, leaves and inflorescences extracts and all their fractions were effective in inhibiting pancreatic lipase. The best anti-obesity potential was demonstrated by the n-hexane and the ethyl acetate fractions of leaves sample, with IC50 values of 0.369±0.020 and 0.336±0.007mg/mL. The same fractions of the inflorescences hydroalcoholic extract were also effective, with IC50 values equal to 0.736±0.045 and 0.780±0.009mg/mL. These results suggest that investigated samples could be a source of interesting compounds able to suppress dietary fat absorption.

Highlights

  • Different drugs, such as dinitrophenol, amphetamines and sibutramine, have been utilized against obesity in the last decades

  • As a continuation of our ongoing studies aimed to find effective antiobesity botanicals (Conforti et al, 2012a; Marrelli et al, 2013, 2014, 2016b, 2016c), here we report the potential anti-obesity activity of Leopoldia comosa (L.) Parl. aerial parts

  • Fresh leaves and inflorescences wild from L. comosa (L.) Parl. were extracted with 70% aqueous EtOH through maceration procedure, and both raw extracts were partitioned between n-hexane, dichloromethane and ethyl acetate

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Summary

Introduction

Different drugs, such as dinitrophenol, amphetamines and sibutramine, have been utilized against obesity in the last decades. Despite some promising results, all of them have been withdrawn because of their serious adverse effects (Marrelli et al, 2016a). Orlistat ((S)-2-formylamino-4-methyl-pentanoic acid (S)-1[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]-methyl]-dodecyl ester) was the only anti-obesity drug approved in Europe for long-term use. This molecule is a chemically synthesized hydrogenated derivative of lipstatin, a natural product of Streptomyces toxytricini. Orlistat acts through the inhibition of gastric and pancreatic lipases, key enzymes for the digestion of dietary triglycerides that form unbound fatty acids from dietary triglycerides that are absorbed at the brush border of the small intestine. Orlistat causes some side effects, such as diarrhea, fecal incontinence and dyspepsia (Marrelli et al, 2016a). From 1998, just few new drugs have been introduced, and the only two available in Europe are naltrexone sustained release (SR)/bupropion SR and liraglutide, recently approved in both USA and Europe (Krentz et al, 2016)

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